A number of long acting narcotic antagonists were synthesized and evaluated in various in vivo and in vitro systems. Several potential stereo-specific, irreversible binding agents to the narcotic receptor were also synthesized and examined in several in vivo and in vitro systems as well as a number of potential anticancer and antiinflammatory agents. Conditions were found for N-demethylation of morphine to normorphine under which no dihydronomorphine (a by-product formerly obtained in 5-10 percent yield) was produced. BIBLIOGRAPHIC REFERENCES: Rice, K.C., Klee, Werner A., Aceto, M.D., Swain, H. H. and Jacobson, A.E.: Potential long acting opiate antagonists: The preparation, pharmacological activity and opiate-receptor binding of of N-substituted 2'-hydroxy-5-methyl-9alpha-propyl-6,7-benzomorphans. J. Pharm. Sci. 66: 193-197, 1977. Rice, K.C., Shiotani, S., Creveling, C.R. and Jacobson, A.E.: N-(2,4,5-Trihydroxyphenethyl) normetazocine: A potential irreversible inhibitor of the narcotic receptor. J. Med. Chem. 20: 673-675, 1977.